1. Pharmacology Introduction

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What does it mean that DR interactions are concentration dependent?
It means that as the concentration of the drug increases the % of receptors bound increases

What does it mean the DR interactions are saturable?
At a certain concentration 100% of receptors will be bound and no matter how much more concentration of drug is added the same number of receptors will still be bound

What is KD?
The Dissociation constant
The likelihood that things will dissociate
The drug concentration required to produce 1/2 max occupancy of the receptor proteins

What is affinity?
The likelihood that things will stay together
1/KD

If KD is very low what does that tell you about the drug?
The drug is not very likely to dissociate (The affinity is high)

If KD is very low what does that tell you about the drug?
It is highly likely to dissociate (The affinity is very low)

What does it mean if a drug has “complete specificity”?
If means there is only 1 specific receptor that will be bound by that drug

Is high affinity (low KD) always a good thing?
No-High affinity with low specificity means it can bind to MANY receptors. Sometimes it is more important to have high specificity

What is B max?
The maximum percentage of receptors that a given drug can bind

What is competitive inhibition of binding?
2 drugs that bind to the same receptor present simultaneously and competing for sites.
The KD will be greater, but the Bmax remains the same

What happens to Kd and Bmax when there is competitive inhibition of binding ?
KD will be greater, but the Bmax remains the same

What is non competitive inhibition?
When drugs bind irreversibly so that other drugs cannot bind
The KD will be the same, but the Bmax is lower (lower max % of receptors that a given drug can bind.

What happens to KD and Bmax when there is non competitive inhibition?
KD will be the same, but B max will be lower (lower max % of receptors that a given drug can bind

What is allosteric modulation binding?
When another substance binds to a modulator (not the same receptor) which either increases or decreases the ability of the other DR to be formed.
The KD can either be larger or smaller, but B max remains the same

What is “Complete Efficacy”?
Maximum response

What does a 30% efficacy mean?
It means that 30% of the max response that can be mediated by a receptor-effector system is mediated

Agonist
Same receptor with a large response (high efficacy)

Partial Agonist
Same receptor with very little response

Antagonist
Same receptor with no response

T/F An Antagonist can have a high affinity, but no Efficacy
True!
Binds to the receptor (Affinity), but doesn’t have any response (efficacy)

What is the potency of a drug?
A relative measure of the concentration/dose of a drug required to produce and effect compared to the concentration or dose required for some other agent

What is EC50?
Excitatory concentration
Concentration of drug required to produce 50% of THAT drugs maximum response

What denotes affinity?
Kd

What denotes potency?
EC50

EC is to potency what Kd is to ____
Affinity

EC is to ____ what Kd is to affinity
Potency

If the Y axis says “Receptors Bound” what is the graph measuring?
Affinity (Kd)

If the Y axis says “Response” what is the graph measuring?
Potency

What is the IC50?
The inhibitory concentration required to produce 50% of THAT drugs response

What is the ED 50?
The dose required to elicit the desired response in 50% of the population

If the Y axis is measuring “Cumulative % Responders” what is the graph measuring?
ED–The dose required to elicit a response

If the therapeutic & toxic graphs are parallel what does this suggest?
If you push the therapeutic effect it becomes toxic

What is the LD?
The Lethal Dose

What is the LD50?
The dose that is lethal in 50% of people

Do you want a high or low therapeutic index?
High!! LD50/ED50 which is the dose that kills/the therapeutic dose

Do you want a high or low standard safety margin?
High! You want the the dose which is effective in 99% of the pop to need to be increased substantially to cause death in 1%

What is the Standard Safety Margin?
The percent by which the dose effective in 99% of the population must increase to cause death in 1% of the population.

What is the therapeutic index?
The LD50 (Lethal does in 50%)/ED50 (Dose that is therapeutic in 50%)

We use cookies to give you the best experience possible. By continuing we’ll assume you’re on board with our cookie policy EC50 the drug concentration giving 50% maximal effect (not binding affinity – the magnitude of a drug effect is …

We use cookies to give you the best experience possible. By continuing we’ll assume you’re on board with our cookie policy Absorption refers to the movement of drug into the bloodstream, with the rate dependent on the physical characteristics of …

We use cookies to give you the best experience possible. By continuing we’ll assume you’re on board with our cookie policy 1. A drug, given as a 100-mg single dose, results in a peak plasma concentration of 20 μg/mL. The …

We use cookies to give you the best experience possible. By continuing we’ll assume you’re on board with our cookie policy Dose response curve shows the relationship between the drug response and the dose Free drug compared to drugs that …

We use cookies to give you the best experience possible. By continuing we’ll assume you’re on board with our cookie policy Drug chemical that interacts with an organism to alter its function, show biolgoical processes and provide methods of diagnosis, …

We use cookies to give you the best experience possible. By continuing we’ll assume you’re on board with our cookie policy Adverse effects General term for undesirable and potentially harmful drug effect Agonist Drug that binds to a receptor and …

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